- Iodine-Mediated Sulfenylation of Imidazo[1,2- a ]pyridines with Ethyl Arylsulfinates
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A simple iodine-mediated approach is reported for the synthesis of sulfenylated imidazo[1,2- a ]pyridines through the reaction of imidazo[1,2- a ]pyridines with ethyl arylsulfinates under mild conditions. The reaction scope was investigated, and a plausible mechanism is proposed to elucidate the reaction process and activation mode. The results indicate that ethyl sulfinates are efficient sulfur sources for the construction of C-S bonds.
- Sun, Jian,Mu, Yangxiu,Iqbal, Zafar,Hou, Jing,Yang, Minghua,Yang, Zhixiang,Tang, Dong
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supporting information
p. 1014 - 1018
(2021/03/15)
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- A mild and chemoselective CALB biocatalysed synthesis of sulfoxides exploiting the dual role of AcOEt as solvent and reagent
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A mild, chemoselective and sustainable biocatalysed synthesis of sulfoxides has been developed exploiting CALB and using AcOEt with a dual role of more environmentally friendly reaction solvent and enzyme substrate. A series of sulfoxides, including the drug omeprazole, have been synthesised in high yields and with excellent E-factors.
- Anselmi, Silvia,Liu, Siyu,Kim, Seong-Heun,Barry, Sarah M.,Moody, Thomas S.,Castagnolo, Daniele
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p. 156 - 161
(2021/01/14)
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- Visible-light-driven electron donor-acceptor complex induced sulfonylation of diazonium salts with sulfinates
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This work reports an efficient sulfonylation reaction enabled by a visible-light-induced radical coupling reaction between phenyl/heterocyclic diazonium salts and sulfinates. Mechanistic experiments disclosed the formation of a versatile electron donor-acceptor (EDA) complex. This transformation is characterized by an easy operational procedure under mild conditions which avoids transition metals, ligands, catalysts, and oxidants.
- Cheng, Lan,Guo, Jianbo,Li, Yufei,Liang, Xin,Wang, Qingmin,Xia, Qing,Zhang, Pei,Zhang, Weihua
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supporting information
p. 8865 - 8870
(2021/11/30)
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- DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA
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Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions co
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- Dihydropyrrolopyridine inhibitors of ROR-gamma
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Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORγ. Also provided are pharmaceutical compositions co
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- Manganese- and Lanthanide-Based 1D Chiral Coordination Polymers as an Enantioselective Catalyst for Sulfoxidation
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The chiral 1D-coordination polymers (CP) {[Ln2(MnLCl)2(NO3)2(dmf)6(H2O)2]·xH2O}n [Ln = Pr (1), Nd (2), Sm (3), and Gd (4)] were synthesized by the reaction of N,N'-bis(4-carboxysalicylidene)cyclohexanediamine (H4L) with [MnCl2·4(H2O)] and [Ln(NO3)3·x(H2O)] in the presence of dmf/pyridine at 90 °C. The polymers consist of manganese-salen-based moieties having carboxylate linkers connected to rare earth atoms in a 1D-chain structure. The polymers are very easily accessible. A one-step synthesis for the ligand and a second step for the preparation of the 1D coordination polymers starting from commercially available material are needed. The solid state structures of 1-4 were established by single-crystal X-ray diffraction. Compounds 1-4 were investigated as heterogeneous catalysts for the sulfoxidation reaction of various alkyl and aryl sulfides. The influence of various solvents and oxidizing agents on the catalytic reaction was examined. It was found that the catalysts were active for more than one reaction cycle without significant loss of activity. For phenylsulfide with 1 mol % of the catalyst 4, a maximum conversion 100% and a chemoselectivity 88% were observed.
- Yadav, Munendra,Bhunia, Asamanjoy,Jana, Salil K.,Roesky, Peter W.
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supporting information
p. 2701 - 2708
(2016/04/05)
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- Application of a novel 1,3-diol with a benzyl backbone as chiral ligand for asymmetric oxidation of sulfides to sulfoxides
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A chiral 1,3-diol with a benzyl backbone has been used for the asymmetric oxidation of sulfides to sulfoxides. Moderate to good yields and enantioselectivity (upto 87% ee) have been observed.
- Gogoi, Paramartha,Kotipalli, Trimurthulu,Indukuri, Kiran,Bondalapati, Somasekhar,Saha, Pipas,Saikia, Anil K.
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supporting information; experimental part
p. 2726 - 2729
(2012/07/17)
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- Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3- methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)
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The design of a new clinical candidate histamine-H3 receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide compounds were modified by re
- Semple, Graeme,Santora, Vincent J.,Smith, Jeffrey M.,Covel, Jonathan A.,Hayashi, Rena,Gallardo, Charlemagne,Ibarra, Jason B.,Schultz, Jeffrey A.,Park, Douglas M.,Estrada, Scott A.,Hofilena, Brian J.,Smith, Brian M.,Ren, Albert,Suarez, Marissa,Frazer, John,Edwards, Jeffrey E.,Hart, Ryan,Hauser, Erin K.,Lorea, Jodie,Grottick, Andrew J.
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supporting information; experimental part
p. 71 - 75
(2012/02/16)
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- INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME
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The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals. The present invention also provides pharmaceutical compositions comprising compounds of formula (4), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formula (4).
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Page/Page column 149
(2008/06/13)
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- 11,21-BISPHENYL-19-NORPREGNANE DERIVATIVES
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The invention relates to a 11,21-bisphenyl-19-norpregnane derivative of formula I STR1 wherein R 1 is selected from H, halogen, (1-6C) alkoxy, and NR 5 R 6, R 5 and R 6 being independently hydrogen or (1-6C)alkyl or R 5 and R 6 together are (3-6C) alkylen
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- A Novel Synthesis of Alkyl Aryl Sulfones via the Telluride Ion-Assisted Coupling of Arenesulfonyl Chlorides with Alkyl Halides
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Arenesulfonyl chlorides undergo a facile one-pot coupling reaction with primary alkyl iodides and benzyl halides through the telluride ion-induced polarity reversal, giving the corresponding alkyl aryl sulfones in acceptable yields.
- Suzuki, Hitomi,Nishioka, Yoshinobu,Padmanabham, Seetharama Iyer,Ogawa, Takuji
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p. 727 - 728
(2007/10/02)
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- Activation of Superoxide. Facile Oxidation of Sulfoxides into Sulfones with a Peroxysulfur Intermediate Generated in situ from 2-Nitrobenzenesulfonyl Chloride and Superoxide
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Various sulfoxides, such as dialkyl, alkyl-aryl, and diaryl sulfoxides, were readily oxidized into the corresponding sulfones, in excellent yields under mild conditions, by 2-nitrobenzene peroxysulfur intermediate generated in situ from 2-nitrobenzene-sulfonyl chloride and potassium superoxide at -30 deg C, in dry acetonitrile.Chemoselective oxidation of sulfoxides which contain both double bond and sulfinyl moiety to the sulfones, was observed under the same conditions.
- KIM, Yong Hae,LEE, Hyeon Kyu
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p. 1499 - 1502
(2007/10/02)
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